tulobuterol / Generic mfg. - LARVOL DELTA

Adjunctive Cilostazol Therapy for Sinus Node Dysfunction After Heart Transplantation. (PubMed, JACC Case Rep) - "Cilostazol may represent an adjunctive option for managing severe SND in heart transplant recipients."

Journal • Transplantation

Thermodynamic and Kinetic Parameters of Four Drugs Toward Beta-2 Adrenergic Receptor Were Measured Robustly and Accurately Through a Chromatographic Column With CotB1 Peptide-Mediated Immobilization. (PubMed, J Sep Sci) - "Two experimental models, such as the injection amount-dependent method and nonlinear chromatography, were employed to measure equilibrium constants and rate constants of four drugs, including bambuterol, salbutamol, clorprenaline, and tulobuterol, toward β2AR. Thermodynamic analysis revealed that four drugs were spontaneously bound to β2AR, and the bindings between them were mainly driven by electrostatic interactions. Our results indicated that the CotB1p-mediated immobilization strategy, resulting in the robust and accurate measurement of the binding parameters of ligand-receptor interaction, will bring new perspectives in applying affinity chromatography in the research fields of drug screening and drug-protein interaction."

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Radical scavenging reactivity of β2-agonists: Mechanistic insights into the antioxidant behavior of salbutamol and tulobuterol. (PubMed, Eur J Pharm Biopharm) - "These results reveal a divergence between thermodynamic preference and kinetic control of radical scavenging and highlight the key role of phenolic functionality in determining the antioxidant behavior of β2-agonists. From a biopharmaceutical perspective, these findings may contribute to a better understanding of the oxidative reactivity and stability of inhaled bronchodilators in pharmaceutical formulations and within the oxidative environment of the respiratory tract."

Journal • Asthma • Immunology • Inflammation • Respiratory Diseases

Development and validation of an LC-MS/MS/MS method for the sensitive quantification of trace β-agonists in complex animal-derived food matrices. (PubMed, Anal Methods) - "To address this drawback, we developed a highly selective and specific liquid chromatography triple-stage tandem mass spectrometry (LC-MS/MS/MS, LC-MS3) method via systematic comparison of MRM and MRM3 modes for the determination of nine β-agonists (ractopamine, penbutolol, cimaterol, salbutamol, clenbuterol, tulobuterol, clorprenaline, terbutaline, and fenoterol) in high-fat milk and pork. In comparison, the conventional LC-MS/MS method showed higher LODs (0.1-0.15 µg kg-1) and LOQs (0.3-0.45 µg kg-1) and broader matrix effects (-18.12-19.35%), confirming the superior sensitivity of the LC-MS3 method. This is the first study to employ MRM3 mode for the determination of β-agonists in high-fat milk and pork matrices."

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Risk assessment and bioaccumulation of β-agonists in the Yellow River Delta of China: Implications for environmental safety. (PubMed, Ecotoxicol Environ Saf) - "Fenoterol was the dominant residue in all samples, 7596.67 ng/kg in sediments, 3657.00 ng/kg in aquatic animals and 65.39 ng/L in water. -terol-type β-agonists exhibited potential bioaccumulation in crab, and notably, tulobuterol exhibited markedly high bioaccumulation in fish...These results indicate the division of functional zones is effective in mitigate the β-agonists pollution. Based on the contamination status of β-agonists in various zones, this study recommends that: Maintain a minimum 2 km buffer between "core zones" and "experimental zones", maintain a minimum 40 km separation between core zones and human activity areas."

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Veterinary Drug Residues in Animal-Origin Food: a UPLC-MS/MS Screening Method for the Determination of 21 Beta-Agonists in Animal Lung and Liver According to Commission Implementing Regulation (EU) 2021/808. (PubMed, J Mass Spectrom) - "With regard to detection capability CCβ, the results obtained permitted the qualitative determination of 11 clenbuterol-like beta-agonists (Clenbuterol, Bromchlorbuterol, Brombuterol, Cimaterol, Cimbuterol, Clenpenterol, Clenproperol, Hydroxymethylclenbuterol, Mabuterol, Mapenterol, Tulobuterol) at 0.05 μg/kg and for 10 salbutamol-like beta-agonists (Carbuterol, Isoxsuprine, Clencyclohexerol, Ractopamine, Ritodrine, Salbutamol, Terbutaline, Zilpaterol, Fenoterol, Salmeterol) at 0.25 μg/kg. The method was validated for lungs and livers of different animal species (cattle, chicken, sheep, and swine): following the requirements of the above-mentioned Regulation. The method was found to be robust and specific."

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Clinical Implications of Mechanical and Adhesive Differences Between Branded and Generic Tulobuterol Patches in Asthma Management. (PubMed, Cureus) - "Conclusion Despite having equivalent pharmacokinetic profiles, branded and generic tulobuterol patches differ in their mechanical and adhesive characteristics, which may influence clinical usability and patient adherence. The results emphasize the importance of considering excipient-driven performance when selecting transdermal products for asthma management."

Journal • Asthma • Immunology • Pulmonary Disease • Respiratory Diseases

Evaluating the safety, tolerability, and efficacy of tulobuterol transdermal patch in patients with asthma or chronic obstructive pulmonary disease: A phase-IV clinical study. (PubMed, Ann Thorac Med) - "Tuloplast™ demonstrated excellent safety, tolerability, and efficacy in improving symptom control and lung function. Its once-daily application enhances adherence, making it a promising alternative for asthma and COPD management."

Journal • P4 data • Asthma • Chronic Obstructive Pulmonary Disease • Immunology • Pediatrics • Pulmonary Disease • Respiratory Diseases

Deep learning-assisted surface-enhanced Raman spectroscopy detection of stimulants. (PubMed, Spectrochim Acta A Mol Biomol Spectrosc) - "This study integrates Surface-Enhanced Raman Spectroscopy (SERS) with deep learning algorithms to achieve high-sensitivity detection and identification of five stimulants, including clorprenaline, propranolol, terbutaline, tulobuterol, and cimaterol. Finally, four machine learning algorithms, support vector machine (SVM), deep neural network (DNN), recurrent neural network (RNN), long short-term memory network (LSTM), were constructed to classify and identify the obtained SERS spectral data, with the LSTM algorithm achieving an identification accuracy of 99.7%. This method holds promise for expansion into trace analysis scenarios such as food detection monitoring and biomarker screening."

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The Efficacy and Safety of Atock Dry Syrup With Acute Bronchitis Patients (clinicaltrials.gov) - P4 | N=296 | Recruiting | Sponsor: SamA Pharmaceutical Co., Ltd | Trial completion date: Aug 2025 ➔ Sep 2027 | Trial primary completion date: Jul 2025 ➔ Jul 2027

Head-to-Head • Trial completion date • Trial primary completion date • Pulmonary Disease • Respiratory Diseases

Ultrasound probe enhanced enzymatic hydrolysis for rapid separation of β2-adrenergic agonists from animal urine and livestock wastewater: Applicability to biomonitoring investigation. (PubMed, Anal Chim Acta) - "Interestingly, since β2-adrenergic agonists are usually considered to be abused mainly in the pig farms, our data indicate that both the detection frequencies and concentrations of these agonists in the ruminant farms were higher than the pig farms. Furthermore, the findings of this work indicated that there is a widespread occurrence of β2-adrenergic agonists in livestock farms, especially for clenbuterol and salbutamol, which may pose both food safety and potential ecological risks. We recommend that stricter controls should be adopted to prevent the illegally usage of these β2-adrenergic agonists in agricultural animals, especially ruminants, and they should also be removed before discharging to the environment."

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Screening for promising multi-target bioactive components from Cortex Mori Radicis for the treatment of chronic cor pulmonale based on immobilized beta1-adrenergic receptor and beta2-adrenergic receptor chromatography. (PubMed, J Chromatogr B Analyt Technol Biomed Life Sci) - "Specific ligands of the two receptors (e.g. esmolol, metoprolol, atenolol, salbutamol, methoxyphenamine, tulobuterol and clorprenaline) were utilized to characterize the specificity and bioactivity of the columns. Molecular docking also indicated that mulberroside C could bind to β2-AR receptor on its agonist site. Taking together, we demonstrated that the chromatographic strategy to identify bioactive natural products based on the β1-AR and β2-AR immobilization, has potential for screening bioactive compounds with multi-targets from complex matrices including traditional Chinese medicines."

Journal • Cardiovascular • Oncology • Respiratory Diseases

A universal method for surface-based binding assays by preparing immobilized β2-adrenergic receptor stationary phase using solid binding peptide as a fusion tag. (PubMed, J Chromatogr A) - "The KAs of salbutamol, chlorprenaline, tulobuterol, and terbutaline on β2AR-CotB1p column were 1.26 × 106, 6.59 × 106, 7.90 × 106, and 8.97 × 105 M-1 respectively, which were two orders of magnitude higher than those on the Halo-β2AR column. The whole immobilization was accomplished within 30 min without the requirement of any special treatment, resulting in enhanced accuracy for determining receptor-ligand binding parameters. Taken together, CotB1p-mediated strategy is simple, rapid, and universal for purification or immobilization of unstable biomolecules like GPCRs for analytical and biological applications."

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Rhamnose-PEG-induced supramolecular helices: Addressing challenges of drug solubility and release efficiency in transdermal patch. (PubMed, J Control Release) - "Pharmacokinetic evaluation demonstrated that the HPR group had >4-fold (Tulobuterol TUL) and 3-fold (Diclofenac DIC) more area under the blood drug concentration curve (AUC) than the commercial TUL and DIC patches in the absence of added excipients and a significantly prolonged mean residence time (MRT) of >4-fold (TUL) and 3-fold (DIC), demonstrating the potential for highly efficacious and prolonged dosing...In summary, HPR enabled a significant simultaneous enhancement of drug loading and drug delivery, which, together with its unique spatial structure, would contribute to the development of TDDS. In addition, the establishment of rhamnose-induced supramolecular helical structures would provide innovative pathways for different drug delivery systems."

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Determination of 14 β-agonists in animal meat by ultra high performance liquid chromatography-tandem mass spectrometry (PubMed, Se Pu) - "In this study, a method based on ultra high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) was established for the rapid detection of 14 β-agonists (clenbuterol, salbutamol, ractopamine, clorprenaline, terbutaline, tulobuterol, bromobuterol, bambuterol, zilpaterol, mabuterol, fenoterol, arformoterol, cimaterol, and cimbuterol) in animal food sources. The results were close to those of the national standard method, indicating that the method is accurate and reliable. Moreover, the proposed method has good stability and high accuracy; thus, it is suitable for the qualitative and quantitative determination of β-agonists in animal meat."

Journal • Cardiovascular • Movement Disorders

Design of a tulobuterol patch with improved mechanical properties: effect of transdermal permeation enhancers on the release process of metal ligand-based acrylic pressure-sensitive adhesives. (PubMed, Drug Deliv Transl Res) - "In addition, AZ increased the mobility of the pressure-sensitive adhesive (PSA) rather than decreasing the drug-PSA interaction, which was the main factor in enhancing TUL release from the patch. In conclusion, a TUL transdermal drug delivery patch was successfully developed using metal-coordinated PSA, and a reference was provided for the design of metal-coordinated acrylic PSA for transdermal patch delivery applications."

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Generic selection criteria for safety and patient benefit [Ⅻ]: Comparing the physicochemical and pharmaceutical properties of brand-name and generic tulobuterol tape. (PubMed, Drug Discov Ther) - "Furthermore, for the stiffness-softness test, a significantly higher value was obtained for each generic yielded compared to Hokunalin (3.7-degree). These factors are important components of product qualities that affect treatment efficacy, including "ease of application" and other usability factors."

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Tulobuterol Patch (Hokunalin Tape)-Induced Leukoderma: A Case Report. (PubMed, Ann Dermatol) - No abstract available

Journal • Dermatology • Vitiligo

Association between use of transdermal tulobuterol and short-term outcomes in patients with stroke and underlying chronic obstructive pulmonary disease: A retrospective cohort study. (PubMed, Medicine (Baltimore)) - "Our study does not support the routine use of transdermal tulobuterol in this patient group. However, further research investigating the long-term efficacy of transdermal tulobuterol in patients with stroke and underlying COPD could help establish its role for the management of these patients."

Journal • Retrospective data • Cardiovascular • Chronic Obstructive Pulmonary Disease • Immunology • Infectious Disease • Pneumonia • Pulmonary Disease • Respiratory Diseases

Tulobuterol Transdermal Patch as an add on therapy in Stable COPD (ERS 2023) - "There would be a subjective improvement with addition of tulobuterol transdermal patch on to triple inhalation therapy for older persons with COPD. Key words : Tulobuterol Transdermal Patch, Long Acting Beta-2 Agonists, Chronic Obstructive Pulmonary Disease.; Pulmonary function testing; Epidemiology; General respiratory patient care; Public health; Physiology"

Chronic Obstructive Pulmonary Disease • Immunology • Pulmonary Disease • Respiratory Diseases

Effect of Tulobuterol Patch Versus Placebo on the Occurrence of Respiratory Adverse Events in Children Undergoing Tonsillectomies: A Randomized Controlled Trial. (PubMed, Anesth Analg) - "In preschool children undergoing tonsillectomy, the preoperative application of a tulobuterol patch could decrease the occurrence of perioperative respiratory adverse events. Further studies are needed to elucidate the effect of the tulobuterol patch in a broad spectrum of pediatric anesthesia."

Adverse events • Journal • Anesthesia • Pediatrics

Protein superglue inspired in-situ one-step site-specific immobilization of beta2-adrenoceptor and its application in bioactive compound screening from Cortex Magnoliae Officinalis. (PubMed, J Chromatogr A) - "The affinity rank order of four ligands to the receptor was tulobuterol> chlorprenaline> salbutamol> terbutaline, which showed highly consistent with data from the radioligand binding assay and the β-AR column prepared by HaloTag technology...Our work unraveled the great potential to generate good bioactivity of the immobilized β-AR through Spy toolbox. This technology can be extended to the immobilization of other functional proteins, providing a better alternative in the field of bioanalysis, biosensing, and separation science."

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Mechanistic insights of different release behaviors dominated by drug physicochemical properties in polyisobutylene pressure sensitive adhesive. (PubMed, Int J Pharm) - "Seven drugs with different physicochemical parameters including clonidine (CLO), flurbiprofen (FLU), diclofenac (DIC), ibuprofen (IBU), zolmitriptan (ZOL), lidocaine (LID), tulobuterol (TUL) and the mixed adhesive (7 : 3, w/w) of Oppanol® B 15 N (M.W. And the trends of in vitro drug release and skin penetration profiles were basically similar. Thus, it was thought that the physicochemical parameters of the drug played a vital role in the drug release behavior of PIB PSAs and would affect the skin penetration process, which provided a reference for the design and application of patches based on PIB PSAs in TDDS."

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Design of a Transdermal Sustained Release Formulation Based on Water-Soluble Ointment Incorporating Tulobuterol Nanoparticles. (PubMed, Pharmaceutics) - "On the other hand, this penetration was significantly inhibited by treatment with a caveolae-mediated endocytosis inhibitor (nystatin). Furthermore, the pathway using caveolae-mediated endocytosis was related to the skin penetration of TUL nanoparticles in the TUL water-soluble ointment with l-menthol. These findings are useful for the design of a transdermal sustained-release formulation based on TUL nanoparticles."

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Development of an Allostery Responsive Chromatographic Method for Screening Potential Allosteric Modulator of Beta2-adrenoceptor from a Natural Product-Derived DNA-Encoded Chemical Library. (PubMed, Anal Chem) - "Under the same conditions, the association constants of three agonists (salbutamol, terbutaline, and tulobuterol) reduced to 47%, 19%, and 27% compared with the data without the inclusion of Cmpd-15 in the mobile phase...Relying on these results, we reasoned that the current method has potential in screening allosteric ligands of the receptor. We expect that it is applicable for the discovery of new allosteric binding sites of a target protein and screening allosteric modulators of the other receptors from complex samples."

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